1,3-비스페닐치오 프로판을 배위자로 한 백금(Ⅱ) 착체의 선택적 세포독성

Selective Cytotoxicity of New Platinum (Ⅱ) Complex Containing 1,3-Bis-phenylthiopropane

A new series of highly water soluble platinum(Ⅱ) complexes {Pt(Ⅱ)[1,3-bis(phenylthio) propane](trans-l-1,2-diaminocyclohexane)(PC-1) and Pt(Ⅱ)[1,3-bis-(phenythio)propane] cis-1,2-diaminocyclohexane(PC-2)} were synthesized, and characterized by their elemental analysis and by various spectroscopic techniques[infrared(IR), 13C-nuclear magnetic resonance (NMR)]. In vitro antitumor activity of new PT(Ⅱ) complexes was tested against P-388 and L-1210 mouse lymphocytic leukemia cell lines, PC-14/P, PC-14/ADM and PC-14/CDDP human pulmonary adenocarcinima, DU-145 human prostate carcinoma, HT-1376 human bladder carcinoma, ZR-75-1 human breast carcinoma, MKN-45/P and MKN-45/CDDP human gastric adenocarcinoma cell lines using colorimetric MTT[3-(4,5-dimethyl thiazol-2-yl)-2,5-diphenyltetrazoliumbromide] assay for cell survival and proliferation. PC-1 showed active against L-1210, P-388 leukemia, human lung, stomach, prostate, bladder and breast cancer cell lines, and the antitumor activity of these compounds were comparable or superior to those of PC-2 and cisplatin. The nephrotoxicities of PC-1 and PC-2 were found quite less than that of cisplatin using MTT and [H] thymidine uptake in rabbit proximal tubule cells and human kidney cortical cells. Based on these results, this novel platinum (Ⅱ) complex compound (PC-1) represents a valuable lead in the development of a new anticancer chemotherapeutic agent capable of improving antitumor activity and low nephrotoxicity.